Ring-opening polymerization of prodrugs: a versatile approach to prepare well-defined drug-loaded nanoparticles.

Journal Article (Journal Article)

The synthesis of polymer-drug conjugates from prodrug monomers consisting of a cyclic polymerizable group that is appended to a drug through a cleavable linker is achieved by organocatalyzed ring-opening polymerization. The monomers polymerize into well-defined polymer prodrugs that are designed to self-assemble into nanoparticles and release the drug in response to a physiologically relevant stimulus. This method is compatible with structurally diverse drugs and allows different drugs to be copolymerized with quantitative conversion of the monomers. The drug loading can be controlled by adjusting the monomer(s)/initiator feed ratio and drug release can be encoded into the polymer by the choice of linker. Initiating these monomers from a poly(ethylene glycol) macroinitiator results in amphiphilic diblock copolymers that spontaneously self-assemble into micelles with a long plasma circulation, which is useful for systemic therapy.

Full Text

Duke Authors

Cited Authors

  • Liu, J; Liu, W; Weitzhandler, I; Bhattacharyya, J; Li, X; Wang, J; Qi, Y; Bhattacharjee, S; Chilkoti, A

Published Date

  • January 2015

Published In

Volume / Issue

  • 54 / 3

Start / End Page

  • 1002 - 1006

PubMed ID

  • 25427831

Pubmed Central ID

  • PMC4293338

Electronic International Standard Serial Number (EISSN)

  • 1521-3773

International Standard Serial Number (ISSN)

  • 1433-7851

Digital Object Identifier (DOI)

  • 10.1002/anie.201409293


  • eng